WO1990012804A3 - Peptides avec des groupes n-terminaux polaires - Google Patents

Peptides avec des groupes n-terminaux polaires Download PDF

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Publication number
WO1990012804A3
WO1990012804A3 PCT/US1990/001764 US9001764W WO9012804A3 WO 1990012804 A3 WO1990012804 A3 WO 1990012804A3 US 9001764 W US9001764 W US 9001764W WO 9012804 A3 WO9012804 A3 WO 9012804A3
Authority
WO
WIPO (PCT)
Prior art keywords
renin
inhibitors
peptides
useful
dependent
Prior art date
Application number
PCT/US1990/001764
Other languages
English (en)
Other versions
WO1990012804A2 (fr
Inventor
Suvit Thaisrivongs
Original Assignee
Upjohn Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Upjohn Co filed Critical Upjohn Co
Priority to KR1019900702636A priority Critical patent/KR920700221A/ko
Publication of WO1990012804A2 publication Critical patent/WO1990012804A2/fr
Publication of WO1990012804A3 publication Critical patent/WO1990012804A3/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0227—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the (partial) peptide sequence -Phe-His-NH-(X)2-C(=0)-, e.g. Renin-inhibitors with n = 2 - 6; for n > 6 see C07K5/06 - C07K5/10
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Peptides à insert à état transitoire non clivable correspondant à la position 10,11 du substrat rénine (angiotensinogène) et comportant un groupe polaire nouveau, correspondant à la formule (L1), où X1 est H2N-, H2NC(CH3)2-, HO2C-, (H2N)(HO2C)CH- ou (HO)2P(O)O-, à la terminaison N du peptide. Ces peptides sont utiles en tant qu'inhibiteurs de rénine et en tant qu'inhibiteurs de protéases rétrovirales. Les inhibiteurs de rénine sont utiles pour diagnostiquer et surveiller l'hypertension due à la rénine, les insuffisances cardiaques, l'hyperaldostéronisme dû à la rénine, et d'autres troubles cardiovasculaires et troubles de la vue dus à la rénine. Les inhibiteurs des protéases rétrovirales, comme la protéase HIV-I, sont utiles pour traiter des maladies provoquées par des rétrovirus, comme le SIDA.
PCT/US1990/001764 1989-04-18 1990-04-05 Peptides avec des groupes n-terminaux polaires WO1990012804A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019900702636A KR920700221A (ko) 1989-04-18 1990-04-05 극성 n-말단기들을 갖는 신규 리닌 억제인자 펩티드

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33975089A 1989-04-18 1989-04-18
US339,750 1989-04-18

Publications (2)

Publication Number Publication Date
WO1990012804A2 WO1990012804A2 (fr) 1990-11-01
WO1990012804A3 true WO1990012804A3 (fr) 1990-11-29

Family

ID=23330419

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1990/001764 WO1990012804A2 (fr) 1989-04-18 1990-04-05 Peptides avec des groupes n-terminaux polaires

Country Status (5)

Country Link
EP (1) EP0468998A1 (fr)
JP (1) JPH04504716A (fr)
KR (1) KR920700221A (fr)
AU (1) AU5407190A (fr)
WO (1) WO1990012804A2 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5554728A (en) * 1991-07-23 1996-09-10 Nexstar Pharmaceuticals, Inc. Lipid conjugates of therapeutic peptides and protease inhibitors
DE4126485A1 (de) * 1991-08-10 1993-02-11 Bayer Ag Trifluormethyl-haltige pseudopeptide
WO1993006127A1 (fr) * 1991-09-17 1993-04-01 Warner-Lambert Company Nouveaux inhibiteurs de renine a base de promedicaments a acides amines
US6071895A (en) * 1992-03-11 2000-06-06 Narhex Limited Polar-substituted hydrocarbons
DE69333270T2 (de) 1992-03-11 2004-08-05 Narhex Ltd. Aminderivate von oxo- und hydroxy- substituierten kohlenwasserstoffen
RU2126794C1 (ru) * 1992-03-11 1999-02-27 Нархекс Лимитед Аминопроизводные оксо- или гидроксизамещенных гидразинов, способ их получения и фармацевтические композиции для ингибирования ретровирусной протеазы
US5888992A (en) * 1992-03-11 1999-03-30 Narhex Limited Polar substituted hydrocarbons
RU94041225A (ru) * 1992-03-25 1996-07-20 Пфайзер Инк. (US) Антивирусные пептиды, способ получения, фармацевтическая композиция, способ лечения ретровирусных инфекций
DE4215874A1 (de) * 1992-05-14 1993-11-18 Bayer Ag Dithiolanylglycinhaltige HIV-Proteaseinhibitoren vom Hydroxyethylenisostertyp

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0104041A1 (fr) * 1982-09-15 1984-03-28 Aktiebolaget Hässle Inhibiteurs d'enzyme
DE3830825A1 (de) * 1987-09-15 1989-03-23 Sandoz Ag Hydrophile reninhemmer, ihre herstellung und verwendung
EP0312157A2 (fr) * 1987-10-13 1989-04-19 Merck & Co. Inc. Inhibiteurs tétrapeptidiques de la rénine, ayant des amides d'acides aminés C-terminaux

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0104041A1 (fr) * 1982-09-15 1984-03-28 Aktiebolaget Hässle Inhibiteurs d'enzyme
DE3830825A1 (de) * 1987-09-15 1989-03-23 Sandoz Ag Hydrophile reninhemmer, ihre herstellung und verwendung
EP0312157A2 (fr) * 1987-10-13 1989-04-19 Merck & Co. Inc. Inhibiteurs tétrapeptidiques de la rénine, ayant des amides d'acides aminés C-terminaux

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Peptides - Chemistry and Biology - Proceedings of the Tenth American Peptide Symposium, 23-28 May 1987, St. Louis, Missouri, US, edited by G.R. Marshall, published by ESCOM, (Leiden, NL), D.J. KEMPF et al.: "Renin Inhibitors based on Novel Dipeptide Analogs: Increased Efficacy through Systematic Inclusion of Polar Functionality", pages 474-475 *

Also Published As

Publication number Publication date
JPH04504716A (ja) 1992-08-20
AU5407190A (en) 1990-11-16
WO1990012804A2 (fr) 1990-11-01
KR920700221A (ko) 1992-02-19
EP0468998A1 (fr) 1992-02-05

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